Abstract

Steroidal spiroazetidinone derivatives ( 3, 10-12 ) were obtained by the multi-step reactions of ketosteroids. It involved Staudinger ketene-imine [2+2] cycloaddition reaction of steroidal iminophenylcholest-5-enes ( 2, 7-9 ). The structural assignment of the products was confirmed on the basis of IR, 1 H NMR, 13 C NMR, MS and analytical data. The synthesized compounds were screened for in vitro antimicrobial activity against different bacterial and fungal strains by agar diffusion method and in vitro antioxidant activity by using DPPH method. Docking studies were performed to investigate the hypothetical binding mode of the steroidal spiroazetidinones. The results suggest that steroidal bearing a core spiroazetidinone scaffold would be potent phramacological agents.

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